Quazepam is a long-acting benzodiazepine used to manage insomnia. It appears to be unique amongst other benzodiazepine derivatives in its relatively high affinity for sleep-promoting α1 subunit-containing GABAA receptors and low affinity for other receptors. It can be found under the brand name Doral. Quazepam is indicated for the treatment of insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Like other benzodiazepines, quazepam likely exerts its effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy. Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha (α) and gamma (γ) subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased. Quazepam is administered as an oral tablet. Possible side effects of using quazepam may include drowsiness, lowered alertness, confusion, and loss of coordination.

Quazepam Pathway References